[CAS NO. 1195765-45-7]  Dabrafenib (GSK2118436)

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PRODUCTS SPECIFICATIONS [1195765-45-7]

Store
Catalog
SLK-S2807
Brand
Selleck
CAS
1195765-45-7

DESCRIPTION [1195765-45-7]

Overview

MDLMFCD17215684
Molecular Weight519.56
Molecular FormulaC23H20F3N5O2S2
SMILESFC1=C(C2=C(SC(C(C)(C)C)=N2)C3=NC(N)=NC=C3)C=CC=C1NS(=O)(=O)C4=C(F)C=CC=C4F

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.9247 mL9.6235 mL19.2471 mL
5 mM0.3849 mL1.9247 mL3.8494 mL
10 mM0.1925 mL0.9624 mL1.9247 mL
50 mM0.0385 mL0.1925 mL0.3849 mL

Description

Dabrafenib (GSK2118436, GSK2118436A) is a mutant specific inhibitor with of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

Targets

B-Raf (V600E) [3]
(Cell-free assay)
B-Raf [3]
(Cell-free assay)
C-Raf [3]
(Cell-free assay)
0.7 nM5.2 nM6.3 nM

In vitro

Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-Raf kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-Raf.


Synonyms

Benzenesulfonamide, N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-
N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
Dabrafenib
GSK 2118436
Dabarefenib
Tafinlar
GSK 436
N-[3-[5-(2-Aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
Tafmlar